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Conformationally constrained o-tolylpiperazine camphorsulfonamide oxytocin antagonists. Structural modifications that provide high receptor affinity and suggest a bioactive conformation.
Williams PD, Ball RG, Clineschmidt BV, Culberson JC, Erb JM, Freidinger RM, Pawluczyk JM, Perlow DS, Pettibone DJ, Veber DF. Williams PD, et al. Among authors: clineschmidt bv. Bioorg Med Chem. 1994 Sep;2(9):971-85. doi: 10.1016/s0968-0896(00)82046-5. Bioorg Med Chem. 1994. PMID: 7712132
Bradykinin agonist activity of a novel, potent oxytocin antagonist.
Pettibone DJ, Clineschmidt BV, Lis EV, Ransom RW, Totaro JA, Young GS, Bock MG, Freidinger RM, Veber DF, Williams PD. Pettibone DJ, et al. Among authors: clineschmidt bv. Eur J Pharmacol. 1991 Apr 24;196(3):233-7. doi: 10.1016/0014-2999(91)90435-s. Eur J Pharmacol. 1991. PMID: 1893911
1-(1-[4-[(N-acetyl-4-piperidinyl)oxy]-2-methoxybenzoyl]piperidin-4- yl)-4H-3,1-benzoxazin-2(1H)-one (L-371,257): a new, orally bioavailable, non-peptide oxytocin antagonist.
Williams PD, Clineschmidt BV, Erb JM, Freidinger RM, Guidotti MT, Lis EV, Pawluczyk JM, Pettibone DJ, Reiss DR, Veber DF, et al. Williams PD, et al. Among authors: clineschmidt bv. J Med Chem. 1995 Nov 10;38(23):4634-6. doi: 10.1021/jm00023a002. J Med Chem. 1995. PMID: 7473590 No abstract available.
1-((7,7-Dimethyl-2(S)-(2(S)-amino-4-(methylsulfonyl)butyramido)bicyclo [2.2.1]-heptan-1(S)-yl)methyl)sulfonyl)-4-(2-methylphenyl)piperaz ine (L-368,899): an orally bioavailable, non-peptide oxytocin antagonist with potential utility for managing preterm labor.
Williams PD, Anderson PS, Ball RG, Bock MG, Carroll L, Chiu SH, Clineschmidt BV, Culberson JC, Erb JM, Evans BE, et al. Williams PD, et al. Among authors: clineschmidt bv. J Med Chem. 1994 Mar 4;37(5):565-71. doi: 10.1021/jm00031a004. J Med Chem. 1994. PMID: 8126695
Identification of an orally active, nonpeptidyl oxytocin antagonist.
Pettibone DJ, Clineschmidt BV, Kishel MT, Lis EV, Reiss DR, Woyden CJ, Evans BE, Freidinger RM, Veber DF, Cook MJ, et al. Pettibone DJ, et al. Among authors: clineschmidt bv. J Pharmacol Exp Ther. 1993 Jan;264(1):308-14. J Pharmacol Exp Ther. 1993. PMID: 8423533
76 results